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    Preparation of oxymorphone from morphine
    2.
    发明授权
    Preparation of oxymorphone from morphine 失效
    从吗啡制备羟吗啡酮

    公开(公告)号：US5922876A

    公开(公告)日：1999-07-13

    申请号：US116284

    申请日：1998-07-16

    申请人： Bao-Shan Huang ,  Yansong Lu ,  Ben-Yi Ji ,  Aris P Christodoulou

    发明人： Bao-Shan Huang ,  Yansong Lu ,  Ben-Yi Ji ,  Aris P Christodoulou

    IPC分类号： A61K20060101 ,  A61K31/485 ,  A61P25/04 ,  C07D20060101 ,  C07D489/02 ,  C07D489/08

    CPC分类号： C07D489/08 ,  C07D489/02

    摘要： A process is provided for preparing oxymorphone from morphine by: (a) reacting morphine with an acyl halide or anhydride to form 3-acylmorphine, or (b) reacting morphine with benzyl-halide to form 3-benzylmorphine, and thereafter either by (3a) or (3b):(3a) introducing a .beta.-oriented hydroxy group at the 14-position of the 3-acyl- or 3-benzyl-morphinone with aqueous hydrogen peroxide and an acid at at temperature of about 15.degree. to about 70.degree. C. to form the 3-acyl or 3-benzyl-14-hydroxymorphinone;(3b) acylating the 3-acyl or 3-benzyl-morphinone with an acylating agent so as to form the dienol acylate followed by oxidizing the dienol acetate to the corresponding 3-acyl or 3-benzyl-14-hydroxymorphinone;(4) hydrogenating the 3-acyl-14-hydroxymorphinone with a catalyst so as to form the 3-acyloxymorphone;(5) hydrolyzing the 3-acyl-oxymorphone with aqueous acidic or basic solution to form oxymorphone;(6) hydrogenating the 3-benzyl-14-hydroxymorphinone with a catalyst so as to form oxymorphone.

    摘要翻译： 提供了通过以下步骤制备吗啡的羟吗啡酮的方法：（a）使吗啡与酰卤或酸酐反应形成3-酰基吗啡，或（b）吗啡与苄基卤反应形成3-苄基吗啡，之后用（3a ）或（3b）：（3a）在3-酰基 - 或3-苄基 - 吗啡酮的14位上用过氧化氢水溶液和酸在约15℃至约70℃的温度下引入β-取代羟基 形成3-酰基或3-苄基-14-羟基吗啡酮; （3b）用酰化剂酰化3-酰基或3-苄基吗啡酮，以形成二烯醇酰化物，然后将乙酸烯醇氧化成相应的3-酰基或3-苄基-14-羟基吗啡酮; （4）用催化剂氢化3-酰基-14-羟基吗啡酮以形成3-酰氧基吗啡酮; （5）用酸性或碱性水溶液水解3-酰基羟基吗啡酮以形成羟吗啡酮; （6）用催化剂氢化3-苄基-14-羟基吗啡酮以形成羟吗啡酮。

    Preparation of oxycodone from codeine
    3.
    发明授权
    Preparation of oxycodone from codeine 失效
    从可待因制备羟考酮

    公开(公告)号：US6008355A

    公开(公告)日：1999-12-28

    申请号：US116283

    申请日：1998-07-16

    申请人： Bao-Shan Huang ,  Yansong Lu ,  Ben-Yi Ji ,  Aris P Christodoulou

    发明人： Bao-Shan Huang ,  Yansong Lu ,  Ben-Yi Ji ,  Aris P Christodoulou

    IPC分类号： A61K20060101 ,  A61K31/485 ,  A61P25/04 ,  C07D20060101 ,  C07D489/02 ,  C07D489/08 ,  C07D471/00

    CPC分类号： C07D489/08 ,  C07D489/02

    摘要： A process is provided for preparing oxycodone from codeine comprising either:(A) the steps of(1) oxidizing codeine so as to form codeinone;(2) converting codeinone to oxycodone in a two-step-one-pot reaction: first reacting codeinone with hydrogen peroxide in water in the presence of an acid at from about 15.degree. to about 70.degree. C. to form 14-hydroxycodeinone and then catalytically hydrogenating 14-hydroxycodeinone in its original reaction mixture to form oxycodone; or(B) the steps of(1) oxydizing codeine so as to form codeinone;(2) reacting codeinone with an acylating agent so as to form codeinone dienol acylate;(3) oxidizing codeinone dienol acylate with an oxidation agent in water or a solubilizing solvent mixture in the presence of an acid at from about 15.degree. to about 70.degree. C. to form 14-hydroxycodeinone;(4) hydrogenating 14-hydroxycodeinone in its original reaction mixture to form oxycodone.

    摘要翻译： 提供了从可待因制备羟可待酮的方法，其包括：（A）步骤（1）氧化可待因以形成可待因酮; （2）将二氢可待因酮转化为两步一锅反应：首先在约15℃至约70℃的酸存在下，将卡知酮与过氧化氢在水中反应，形成14-羟可待因酮，然后 在其原始反应混合物中催化氢化14-羟可待因酮以形成羟考酮; 或（B）步骤（1）氧化可待因以形成可待因酮; （2）将代森西酮与酰化剂反应，形成可酮二酮二烯醇酰化物; （3）在约15℃至约70℃的酸存在下，用氧化剂在水或增溶溶剂混合物中氧化可待因酮二烯醇酰化物以形成14-羟可待因酮; （4）在其原始反应混合物中氢化14-羟可待因酮以形成羟考酮。

    Preparation of naltrexone from codeine and 3-benzylmorphine
    5.
    发明授权
    Preparation of naltrexone from codeine and 3-benzylmorphine 失效
    从可待因和3-苄基吗啡制备纳曲酮

    公开(公告)号：US6013796A

    公开(公告)日：2000-01-11

    申请号：US116282

    申请日：1998-07-16

    申请人： Bao-Shan Huang ,  Yansong Lu ,  Ben-Yi Ji ,  Aris P Christodoulou

    发明人： Bao-Shan Huang ,  Yansong Lu ,  Ben-Yi Ji ,  Aris P Christodoulou

    IPC分类号： A61K20060101 ,  A61K31/485 ,  A61P25/04 ,  C07D20060101 ,  C07D489/02 ,  C07D489/08 ,  C07D413/00 ,  C07D471/00

    CPC分类号： C07D489/08 ,  C07D489/02

    摘要： For the synthesis of 3-methylnaltrexone from codeine in this invention, codeine is converted to 6-acetylcodeine, which is N-demethylated to 6-acetylcodeine hydrochloride, followed by alkylating the nitrogen to form 17-cyclopropylmethylnorcodeine. The latter is oxidized to 17-cyclopropylmethylnorcodeinone. For the synthesis of naltrexone from morphine in this invention, morphine is converted to 3-benzylnormorphine as described above in the synthesis of noroxymorphone. 3-Benzylnormorphine is reacted with cyclopropylmethyl halide to produce 3-benzyl-17cyclopropylmethylnormorphine, a novel compound, which is oxidized to 3-benzyl-17-cyclopropylmethyl-normorphinone, a novel compound, by Swern oxidation.

    摘要翻译： 为了合成本发明可待因的3-甲基纳曲酮，将可待因转化为6-乙酰基可待因，将其N-去甲基化为6-乙酰基可待因盐酸盐，然后将氮烷基化形成17-环丙基甲基可待因。 后者被氧化成17-环丙基甲基可待因酮。 为了在本发明中从吗啡合成纳曲酮，如上所述在去甲吗啡酮的合成中，吗啡被转化为3-苄基吗啡。 3-苄基吗啡与环丙基甲基卤反应生成3-苄基-17环丙基甲基吗啡，一种新型化合物，通过Swern氧化被氧化成3-苄基-17-环丙基甲基 - 正吗啡酮，一种新型化合物。

    Preparation of 14-hydroxynormorphinones from normorphinones
    6.
    发明授权
    Preparation of 14-hydroxynormorphinones from normorphinones 失效
    从正诺酮制备14-羟基吗啡酮

    公开(公告)号：US5952495A

    公开(公告)日：1999-09-14

    申请号：US116286

    申请日：1998-07-16

    申请人： Bao-Shan Huang ,  Yansong Lu ,  Ben-Yi Ji ,  Aris P Christodoulou

    发明人： Bao-Shan Huang ,  Yansong Lu ,  Ben-Yi Ji ,  Aris P Christodoulou

    IPC分类号： A61K20060101 ,  A61K31/485 ,  A61P25/04 ,  C07D20060101 ,  C07D489/02 ,  C07D489/08 ,  C07D413/00 ,  C07D471/00

    CPC分类号： C07D489/08 ,  C07D489/02

    摘要： A process is provided for preparing 14-hydroxynormorphinones having the formula: ##STR1## which comprises reacting normorphinones having the formula: ##STR2## wherein R is selected from the group consisting of lower alkyl of 1 to 7 carbon atoms, cycloalkyl-lower alkyl with 3-6 ring carbon atoms, benzyl and a substituted-benzyl having the formula: ##STR3## wherein Q and Q.sup.1 are individually selected from the group consisting of hydrogen, lower alkyl, trifluoromethyl, nitro, dialkylamino and cyano;R' is selected from the group consisting of R, 2-(4-morpholinyl)ethyl, benzyloxy carbonyl and R"C(O)-- wherein R" is lower alkyl of 1-4 carbon atoms;with hydrogen peroxide at a temperature of from about 15.degree. C. to about 70.degree. C. in the presence of an acid and an aqueous solvent system to solubilize the reactant for a period of time so as to form the 14-hydroxynormorphinones.

    摘要翻译： 提供了一种制备具有下式的14-羟基吗啡酮的方法：其包括使具有下式的正诺酮：其中R选自1至7个碳原子的低级烷基，具有3-6个环碳原子的环烷基 - 低级烷基 苄基和具有下式的取代的苄基：其中Q和Q 1分别选自氢，低级烷基，三氟甲基，硝基，二烷基氨基和氰基; R'选自R，2-（4-吗啉基）乙基，苄氧基羰基和R''C（O） - ，其中R“为1-4个碳原子的低级烷基; 与过氧化氢在约15℃至约70℃的温度下，在酸和水性溶剂体系的存在下，使反应物溶解一段时间，以形成14-羟基吗啡酮。